Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents.
The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, a series of new class of hybrid 4-aminoquinoline triazines were synthesized and screened against CQ sensitive strain 3D7 of P. falciparum in an in vitro model. Compounds 65 and 69 exhibited more than 99% suppression on day 4 and on day 6 post treatment, compound 69 showed impressive 99.11% suppression against CQ resistant strain N-67 of P. yoelii in an in vivo assay.
Kumar
Ashok
A
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Srivastava
Kumkum
K
Raja Kumar
S
S
Puri
S K
SK
Chauhan
Prem M S
PM
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002738:Chloroquine / Q000737:chemistry; D015195:Drug Design; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000378:metabolism; D010967:Plasmodium yoelii / Q000378:metabolism; D002727:Proguanil / Q000737:chemistry; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000634:Aminoquinolines; D000962:Antimalarials; D014227:Triazines; C026009:cycloguanil; D002738:Chloroquine; D002727:Proguanil